GABA Receptor
Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor
GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). It has long been recognized that the fast response of neurons to GABA that is blocked by bicuculline and picrotoxin is due to direct activation of an anion channel. This channel was subsequently termed the GABAA receptor. Fast-responding GABA receptors are members of family of Cys-loop ligand-gated ion channels. A slow response to GABA is mediated by GABAB receptors, originally defined on the basis of pharmacological properties.
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GABA Receptor Inhibitors
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GABA Receptor Agonists
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GABA Receptor Antagonists
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GABA Receptor Activators
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GABA Receptor Modulators
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GABA Receptor Controls
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GABA Receptor Ligands
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GABA Receptor Related Products (782)
Related Products (782)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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Cyclothiazide (Standard)
0 ImagesCat. No.: HY-101165RCAS No.: 2259-96-3Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures.
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SKF 89976A
0 ImagesCat. No.: HY-100228CAS No.: 85375-85-5SKF89976A is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.
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3-Hydroxy desalkylflurazepam
0 ImagesCat. No.: HY-171028CAS No.: 17617-60-63-Hydroxy desalkylflurazepam is a benzodiazepine with potential sedative and anxiolytic effects.
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GABRA5 modulator-1
0 ImagesCat. No.: HY-186006CAS No.: 207307-48-0GABRA5 modulator-1 is a GABRA5 modulator.
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Picrotoxinin (Standard)
0 ImagesCat. No.: HY-B1494RCAS No.: 17617-45-7Picrotoxinin (Standard) is the analytical standard of Picrotoxinin. This product is intended for research and analytical applications. Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.
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THIP (hydrobromid)
0 ImagesCat. No.: HY-10232ACAS No.: 65202-63-3Synonyms: Gaboxadol (hydrobromid)THIP (Gaboxadol) hydrobromide is a blood-brain barrier-penetrant, orally active selective GABAA receptor agonist. THIP hydrobromide exhibits EC50 values of 33 μM and 130 μM for α4β2δ and α4β1δ receptors, respectively. THIP hydrobromide activates extrasynaptic GABAA receptors to produce tonic inhibition and inhibits GABAergic interneurons to cause disinhibition. THIP hydrobromide is used in research on insomnia, sleep disorders, and addictive behaviors.
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Dipropofol (Standard)
0 ImagesDipropofol (Standard) is the analytical standard of Dipropofol. This product is intended for research and analytical applications. Dipropofol is a dimeric derivative of Propofol (HY-B0649) with antioxidant and antibacterial activities. Dipropofol terminates free radical chain reactions, scavenges DPPH free radicals and inhibits lipid peroxidation. Dipropofol protects cells from death induced by glutamate, Aβ(25-35) and buthionine sulfoximine, and increases the survival rate of mice exposed to oxygen. Dipropofol selectively activates tonic GABAA currents, hyperpolarizes resting membrane potential, reduces action potential firing, and alleviates the severity of seizures induced by Kainic acid. Dipropofol can be used in the research of Gram-positive bacterial infections, Alzheimer's disease, cerebral ischemia-related neuronal injury, oxygen toxicity and temporal lobe epilepsy.
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Bicuculline methiodide (Standard)
0 ImagesCat. No.: HY-103474RCAS No.: 40709-69-1Synonyms: (-)-Bicuculline methiodide (Standard)Bicuculline methiodide (Standard) is the analytical standard of Bicuculline methiodide (HY-103474). This product is intended for research and analytical applications. Bicuculline methiodide ((-)-Bicuculline methiodide) is a potent GABAA blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.
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Tiagabine-d4
0 ImagesCat. No.: HY-B0696S1Synonyms: NO050328-d4; NO328-d4; TGB-d4Tiagabine-d4 (NO050328-d4) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.
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MIDD0301 sodium
0 ImagesCat. No.: HY-123801ACAS No.: 2593569-36-7Synonyms: GL-II-93 sodiumMIDD0301 (GL-II-93) is an orally available, active γ-aminobutyric acid type A receptor (GABAAR) inhibitor and anti-asthmatic agent. MIDD0301 exhibits biological and immunotoxicological safety in mice and does not affect the number of circulating lymphocytes, monocytes, and granulocytes. MIDD0301 has no significant adverse immune response at repeated doses, which is better than Prednisone (HY-B0214). MIDD0301 relaxes histamine-contracted guinea pig and human airway smooth muscle and is used in the study of bronchoconstrictive diseases.
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DMCM hydrochloride (Standard)
0 ImagesCat. No.: HY-100369ARCAS No.: 1215833-62-7DMCM (hydrochloride) (Standard) is the analytical standard of DMCM (hydrochloride). This product is intended for research and analytical applications. DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 ?receptors, respectively.
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Rilmazafone hydrochloride (Standard)
0 ImagesCat. No.: HY-U00228RCAS No.: 85815-37-8Synonyms: 450191S (Standard)Rilmazafone hydrochloride (450191S) is a benzodiazepine (omega) ligand.
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Progabide (Standard)
0 ImagesSynonyms: SL 76002 (Standard)Progabide (Standard) is the analytical standard of Progabide. This product is intended for research and analytical applications. Progabide is a gamma-aminobutyric acid receptor (GABA) agonist.
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Radequinil (Standard)
0 ImagesCat. No.: HY-106025RCAS No.: 219846-31-8Synonyms: AC-3933 (Standard)Radequinil (Standard) is the analytical standard of Radequinil (HY-106025). This product is intended for research and analytical applications. Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively.
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Inaperisone
0 ImagesInaperisone is a centrally acting muscle relaxant. Inaperisone can inhibit the micturition reflex by acting indirectly on GABAB receptors in the brainstem.
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Chlormezanone (Standard)
0 ImagesChlormezanone (Standard) is the analytical standard of Chlormezanone. This product is intended for research and analytical applications. Chlormezanone resembles benzodiazepine. The action of Chlormezanone is similar to benzodiazepine-type agents. Chlormezanone is used as an anxiolytic and a muscle relaxant.
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3-Carene (Standard)
0 ImagesCat. No.: HY-N6663RCAS No.: 13466-78-93-Carene (Standard) is the analytical standard of 3-Carene (HY-N6663). This product is intended for research and analytical applications. 3-Carene is an orally active TCA cycle enzyme inhibitor. 3-Carene inhibits succinate dehydrogenase and malate dehydrogenase as well as pyruvate kinase, disrupting energy metabolism. 3-Carene disrupts cell wall and cell membrane integrity, leading to potassium ion leakage, protein leakage, membrane depolarization, ATP depletion, morphological disruption, and cell lysis. 3-Carene interferes with amino acid metabolism, pantothenate and CoA biosynthesis, purine and pyrimidine metabolism, and aminoacyl-tRNA biosynthesis. 3-Carene enhances GABA receptor-mediated synaptic responses. 3-Carene can be used in research on bacterial infections, inflammation, anxiety, and sleep disorders.
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Epiallopregnanolone-d5
0 ImagesCat. No.: HY-124463S1Synonyms: 5α,3β-THDOC-d5Epiallopregnanolone-d5 (5α,3β-THDOC-d5) is deuterium labeled Epiallopregnanolone. Epiallopregnanolone (5α,3β-THDOC), a 3β-hydroxy neurosteroid, an antagonist at GABAA receptors and a NMDA receptor enhancer.
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Lofendazam
0 ImagesCat. No.: HY-184368CAS No.: 29176-29-2Lofendazam is a major metabolite of Arfendazam. Lofendazam acts as a positive allosteric modulator/partial agonist of GABAa receptor, with IC50 values of 10.1 nM and 9.1 nM in bovine cerebral cortex and bovine cerebellum, respectively; its in vivo ED50 via oral administration is 233 µmol/kg.
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D-DABA
0 ImagesCat. No.: HY-W291165CAS No.: 26908-94-1Synonyms: D-2,4-Diaminobutyric acidD-DABA is the enantiomeric form of L-DABA. D-DABA is also a weak inhibitor of GABA-T, but which has only one twentieth of the potency of the L-isomer in inhibiting GABA uptake.
